PROBLEM TO BE SOLVED: To solve a problem in which only a small amount of medicine arrives at a site of action, and the medicine may cause a side effect on the healthy tissue of the body on te basis of the distribution thereof.SOLUTION: There is provided a method for producing injectable medicament preparations containing a therapeutically and/or diagnostically effective substance which comprises an active agent, a spacer molecule, and at least one protein-binding molecule. After being added to the body, the therapeutically and/or diagnostically effective substance covalently bonds to the body fluid or tissue constituents via the protein-binding molecule, thus providing a form of transport of the active agent that can be hydrolytically or enzymatically cleaved, according to pH, in the body while releasing the active agent.【課題】薬剤のほんの少量が作用部位に到達し、薬剤は、その分布に基づき、身体の健康な組織上に副作用を引き起こすことが起こる。【解決手段】本発明は、作用物質、スペーサー分子及び少なくとも１種の蛋白質結合性分子から成り、身体に加えた後に、蛋白質結合性分子を介して体液－又は組織成分に共有結合する、治療的及び／又は診断的に有効な物質を含有する注射可能な医薬調製剤の製法に関し、従って、ｐＨ‐依存的、加水分解的又は酵素的に身体中で、作用物質の遊離下に分解可能である作用物質の輸送形が存在する。【選択図】なし
